DNA-encoded focused indazole library synthesis by a palladium- mediated C-N(sp(2)) cross-coupling reaction between DNA-linked (hetero)aryl halides and aromatic nitrogen heterocycles
文献类型：期刊论文
| 作者 | Yang, Juan3,5; Xia, Shengdi4; Liu, Jiaxiang2; Yu, Zikun2; Mei, Lianghe1; Lu, Weiwei5; Chen, Yulin1; Chen, Shaopeng1; Wang, Xuan5; Lu, Xiaojie3,4,5
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| 刊名 | TETRAHEDRON LETTERS
 |
| 出版日期 | 2022-04-27 |
| 卷号 | 96页码:6 |
| ISSN号 | 0040-4039 |
| DOI | 10.1016/j.tetlet.2022.153732 |
| 通讯作者 | Lu, Xiaojie(xjlu@simm.ac.cn) |
| 英文摘要 | Incorporating various heteroaryl motifs into small-molecule moieties of DNA-encoded libraries is beneficial to support hit identification. More privileged heterocycles based libraries are urgently needed to expand the chemical space of the DNA encoded library. Because currently published on-DNA C-N cross-coupling methods mainly focused on exocyclic aromatic amines, lacking systematic investigation for incorporating pharmaceutically valuable N-aryl hetero-aromatic moiety into DNA-encoded libraries, in this paper, we have reported an on-DNA protocol to attach the DNA-linked electrophiles to the (H)N- heteroaryl rings. This method could translate the monofunctional heteroaryl agents into "bifunctional building blocks ", which have been applied for the DNA encoded focused indazole library synthesis. (C) 2022 Elsevier Ltd. All rights reserved. |
| WOS关键词 | ARYLATION ; CHEMISTRY ; BROMIDES ; PD |
| 资助项目 | Shanghai Municipal Science and Technology Major Project[NSFC-91953203] ; Shanghai Municipal Science and Technology Major Project[NSFC-21877117] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| WOS记录号 | WOS:000803841500010 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/301404]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Lu, Xiaojie |
| 作者单位 | 1.Chinese Acad Sci, Suzhou Inst Drug Innovat, Shanghai Inst Mat Med, 108 Yuxin Rd, Suzhou City 215123, Jiangsu Provinc, Peoples R China 2.Alphama Biotechnol Suzhou Co Ltd, 108 Yuxin Rd, Suzhou City 215123, Jiangsu Provinc, Peoples R China 3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China 4.Nanjing Univ Chinese Med, Sch Chinese Mat Med, 138 Xianlin Rd, Nanjing 210023, Peoples R China 5.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 501 Haike Rd,Zhang Jiang Hitech Pk, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, Juan,Xia, Shengdi,Liu, Jiaxiang,et al. DNA-encoded focused indazole library synthesis by a palladium- mediated C-N(sp(2)) cross-coupling reaction between DNA-linked (hetero)aryl halides and aromatic nitrogen heterocycles[J]. TETRAHEDRON LETTERS,2022,96:6. |
| APA | Yang, Juan.,Xia, Shengdi.,Liu, Jiaxiang.,Yu, Zikun.,Mei, Lianghe.,...&Lu, Xiaojie.(2022).DNA-encoded focused indazole library synthesis by a palladium- mediated C-N(sp(2)) cross-coupling reaction between DNA-linked (hetero)aryl halides and aromatic nitrogen heterocycles.TETRAHEDRON LETTERS,96,6. |
| MLA | Yang, Juan,et al."DNA-encoded focused indazole library synthesis by a palladium- mediated C-N(sp(2)) cross-coupling reaction between DNA-linked (hetero)aryl halides and aromatic nitrogen heterocycles".TETRAHEDRON LETTERS 96(2022):6. |
入库方式： OAI收割
来源：上海药物研究所
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